Home Tools

SAFit2

Catalog No. T16836 CAS 1643125-33-0

SAFit2 is a highly effective and selective fk506 binding protein 51(FKBP51) inhibitor (Ki: 6 nM). SAFit2 can enhance AKT2-AS160 binding and participate in the downstream response of glucocorticoid release in vivo, and is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SAFit2, CAS 1643125-33-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 80.00
5 mg	In stock	$ 197.00
10 mg	In stock	$ 297.00
25 mg	In stock	$ 493.00
50 mg	In stock	$ 718.00
100 mg	In stock	$ 993.00
1 mL * 10 mM (in DMSO)	In stock	$ 262.00

Bulk Inquiry

Select Batch

Purity: 99.74%

ee: 98.82%

Purity: 98.52%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SAFit2 is a highly effective and selective fk506 binding protein 51(FKBP51) inhibitor (Ki: 6 nM). SAFit2 can enhance AKT2-AS160 binding and participate in the downstream response of glucocorticoid release in vivo, and is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.
Targets&IC50	FKBP51:6 nM(ki)
In vitro	SAFit2 treatment enhances pAKT2 expression in the soleus and EDL muscle, as well as pAS160 expression in the EDL muscle of WT cells, while FKBP51 antagonism has no impact on 51KO cells. Additionally, SAFit2 treatment leads to an increase in membrane-bound GLUT4 expression in primary EDL myotubes from WT mice, whereas no such effect is observed in 51KO mice.[1]
In vivo	SAFit2 significantly enhances phosphorylation of AKT2 and AS160 in the EDL muscle, while also increasing GLUT4 expression at the muscle membrane in the soleus. Administration of SAFit2 induces an anxiolytic phenotype in mice tested 16 hours after injection, as evidenced by a significant increase in open arm time in the elevated plus maze (EPM) (z=-2.183, p<0.05). SAFit2 treatment results in a significantly decreased latency to enter the lit compartment (z=-2 to 265, p<0.05), as well as a notable increase in distance, traveled (t(20)=-2.371, p<0.05) within the lit compartment. It has been observed that 30 days of SAFit2 administration leads to reduced body weight in both control and high-fat diet conditions. When SAFit2 is administered 1 hour before testing, no changes in anxiety-related behavior are detected.[1][2]

Molecular Weight	802.99
Formula	C46H62N2O10
CAS No.	1643125-33-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (112.1 mM), Sonication is recommended.

References and Literature

1. Balsevich G, et al. Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function. Nat Commun. 2017 Nov 23;8(1):1725. 2. Hartmann J, et al. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties. J Neurosci. 2015;35(24):9007-9016. 3. Gaali S,et al. Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51. J Med Chem. 2016;59(6):2410-2422.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

FKBP51F67V-selective antagonist Ligand2

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SAFit2 1643125-33-0 Apoptosis Autophagy Immunology/Inflammation FKBP SAFit-2 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.